Discovery of R-142086 as a factor Xa (FXa) inhibitor: syntheses and structure-activity relationships of cinnamyl derivatives.

  title={Discovery of R-142086 as a factor Xa (FXa) inhibitor: syntheses and structure-activity relationships of cinnamyl derivatives.},
  author={Tetsuji Noguchi and Naoki Tanaka and Toyoki Nishimata and Riki Goto and Miho Hayakawa and Atsuhiro Sugidachi and Taketoshi Ogawa and Yoichi Niitsu and Fumitoshi Asai and Tomoko Ishizuka and Koichi Fujimoto},
  journal={Chemical \& pharmaceutical bulletin},
  volume={57 1},
To develop a novel and effective anticoagulant with potent and selective factor Xa (FXa) inhibitory activity, a new series of cinnamyl derivatives with enhanced lipophilicity and prodrug forms were synthesized and their biological activities were evaluated. As a result, we found that cinnamyl derivative (N-[4-[1-(acetimidoyl)piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid dihydrochloride (26d, R-142086) with a fluorine atom on the… 

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